Tifental, a new class 1.1 drug of Guizhou bailing chemical, has been granted a US patent

Guizhou bailing (002424) announced in the evening of June 14 that the company's new chemical 1.1 drug, tefentai (original Y101), had recently obtained a US patent Tifentai US patent application No is 12 / 056506, patent authorization date is May 5, 2015, Announcement No is No us9023809 B2, and the applicant is the Key Laboratory of natural product chemistry, Chinese Academy of Sciences, Guizhou Province, Tianjin Pharmaceutical Research Institute, and 302 Hospital of Chinese people's Liberation Army According to the technical cooperation and development contract signed between the company and the Key Laboratory of natural product chemistry of Guizhou Academy of Sciences, Tianjin Pharmaceutical Research Institute and 302 Hospital of the people's Liberation Army, Guizhou bailing has the patent right of tifentai (original Y101) Now the company has officially obtained the U.S patent authorization certificate of tifentai, a new chemical drug of category 1.1 Both parties will sign a supplementary agreement as soon as possible to confirm Protect the patent right of Guizhou bailing to tifentai (original Y101)     It is reported that the patent obtained by tifentai in the United States is that after the company published the paper "evaluation of the hypoglycemic effect of tangningtongluo on two animal models" in the international well-known medical journal Journal Journal of diabetes research in September 2014, Guizhou bailing obtained international recognition again in the research of Miao medicine preparation, reflecting that the company is an excellent national medicine Contribution to the world Tifentai is a new chemical drug of anti hepatitis B virus 1.1, CO developed by Guizhou bailing, together with the Key Laboratory of natural product chemistry of Chinese Academy of Sciences, Tianjin Pharmaceutical Research Institute and 302 Hospital of the people's Liberation Army It belongs to the field of national key prevention and control of infectious diseases, and continues to win the national "11th Five Year Plan", "12th Five Year Plan" major new drug creation and Guizhou Provincial heavy duty The support of large-scale science and technology projects is the first class 1.1 new chemical medicine with completely independent intellectual property rights at home and abroad in Guizhou Province According to the announcement, Guizhou bailing bears the costs of preclinical research, clinical research and related patent transfer needed for the development of tifentai According to the contract, we have the patent and production approval documents of tifentai, and we have the new drug certificate of tifentai together with three research units Hepatitis B (abbreviated as hepatitis B) is a serious disease that endangers human health and can lead to liver cancer and cirrhosis There are a large number of hepatitis B patients and hepatitis B virus carriers in the world, with more than 120 million people in China alone At present, there are no drugs that can cure hepatitis B completely in the world Compared with the drugs for other diseases, there are relatively few kinds of drugs for clinical treatment, mainly including lamivudine, adefovir dipivoxil, entecavir and interferon The clinical doctors are often at a loss and the psychological and economic burden of patients are also increased Therefore, it is not only the expectation of doctors and patients, but also the responsibility of drug technologists to develop new anti HBV drugs with new skeleton and new target Since the 1990s, Professor Liang Guangyi, the Key Laboratory of natural product chemistry of Guizhou Academy of Chinese sciences, has devoted himself to studying the active ingredients of horseshoe gold, a folk medicine of Miao Nationality in Guizhou Province, which is used to treat hepatitis In 1999, the National Natural Science supported the research on derivatives of horseshoe gold lead compound, which started the development of tifentai Liu Changxiao, academician of Chinese Academy of engineering, who is responsible for the preclinical study of pharmacokinetics and toxicology of tifental, said that "tifental" is a new structure dipeptide compound Preclinical studies showed that the mechanism of anti HBV was different from that of the existing drugs, there was no obvious rebound after discontinuation of the drug, and it had a strong inhibitory effect on the resistant strains of nucleoside analogues Tiffany has a new mechanism and is expected to solve the world's problems "Through the study of mechanism of action, it is shown that the action site of" tifentai "against hepatitis B virus is not to inhibit the expression of pgRNA (pre transcriptional genome) or the activity of DNA polymerase, it may achieve anti HBV function by inhibiting cccDNA (covalently closed cyclic deoxyribonucleic acid), but it needs to be confirmed by further mechanism and clinical research." According to the public data, cccDNA is the original synthetic template of HBV pre genome RNA replication, and is the key factor of HBV persistent infection Only by clearing cccDNA can we completely eliminate the virus carrying status of hepatitis B patients, which is the goal of anti hepatitis B treatment Xia Wen, R & D director of Guizhou bailing Group Pharmaceutical Co., Ltd., said that horseshoe gold is commonly used by Miao people in Guizhou to treat hepatitis Tiffental is the effective part of horseshoe gold, which has strong inhibition on hepatitis B virus Horseshoe gold element was separated and a number of compounds were successfully synthesized and derived by using modern drug synthesis technology Through the screening of the national new drug screening center, on the basis of full evaluation of safety, effectiveness, controllability and stability, it was decided to take the compound No.: Y101 (named as: tefentai at the time of new drug application) as an alternative drug for preclinical research According to FDA data, nearly 30% of the 1600 new drugs approved in the United States in the past 30 years are from natural drugs Guizhou bailing has been in charge of the research on tifentai since 2009, which lasted for more than three years At the end of 2012, it successfully completed the preclinical research; in February 2013, it applied to CFDA for new drug application according to the standard of 1.1 chemical new drugs; in January 2014, tifentai and its preparations passed the review once and obtained the clinical trial approval issued by CFDA; after nearly half a year's preparation, from May 2014, The first phase of clinical research began in tifentai, and the research progress is smooth Compared with traditional Chinese medicine preparations, the biggest difference in the research and development route of tfental is that most of the traditional Chinese medicine is the superposition of multiple herbs, while tfental is the stripping of effective ingredients "In the past, due to the influence of backward scientific and technological means and productivity, almost all the prescriptions of traditional Chinese medicine were based on the function of monarch medicine, adding minister medicine, adjuvant, so that the medicine can enhance the curative effect and reduce the toxicity, and gradually formed a large compound This kind of medicine obtained through" addition "is difficult to use the modern scientific system to establish a perfect quality standard However, with the continuous progress of science and technology, through the analysis of the ingredients in the monarch drug, using purification and separation technology and combined with biotechnology to obtain the active ingredients that are suitable for the main function and treatment, after manual spectrum analysis, using pharmaceutical chemical technology to synthesize and get new compounds, and finally locking the alternative compounds through the drug-forming experiment This subtraction method can not only effectively use and protect the medicinal materials, but also obtain new drug resources through scientific evaluation system The research and development of tifentai is a process from discovery to invention Through continuous separation and purification, the purity of new compounds can reach more than 99.8% It embodies the use of modern pharmaceutical technology to sublimate "traditional Miao medicine" into "science and technology Miao medicine" and has been recognized by the international community If Tiffany succeeds in research and development, it will benefit all mankind " Xia Wen said so The "one, two, two" technological innovation system, which helps to build the "one, two, two" technological system for scientific research and development, provides Guizhou bailing with a strong research carrier and R & D team, promotes the formation of the company's talent echelon, and can better provide guarantee and support for the company's R & D " Guizhou bailing Dong Mi Niu min concluded "One, two" technological innovation system refers to one national enterprise technology center, two hardware research platforms and two software research platforms The two hardware research platforms are the national medicine (traditional Chinese Medicine) compound preparation engineering technology research center jointly established with Guiyang University of traditional Chinese medicine and the national medicine (traditional Chinese Medicine) oral preparation manufacturing technology engineering research center jointly established with Guizhou University The two software research platforms are National Postdoctoral research workstation and academician workstation